2-Chloroacetaldehyde, a metabolite of cyclophosphamide in the rat

Abstract

1. Following simultaneous i.v. administration of a mixture of [4-¹⁴C]cyclophosphamide (¹⁴C-CP) and [side-chain³H]CP to rats, a metabolite containing predominantly ³H radioactivity was excreted in the urine. 2. The ³H-labelled urinary metabolite was identified as 2-chloroacetaldehyde. 3. Chloro[³H]acetaldehyde accounted for approx. 3.8% of urinary³H radioactivity. 4. The importance of chloroacetaldehyde as a toxic metabolite of CP is discussed. particularly in relation to haemorrhagic bladder disease.